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首页> 外文期刊>Asian Journal of Pharmaceutical Sciences >Cooperative effect of polyvinylpyrrolidone and HPMC E5 on dissolution and bioavailability of nimodipine solid dispersions and tablets
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Cooperative effect of polyvinylpyrrolidone and HPMC E5 on dissolution and bioavailability of nimodipine solid dispersions and tablets

机译：聚乙烯吡咯烷酮和HPMC E5对尼莫地平固体分散体和片剂的溶解和生物利用度的协同作用

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Solid dispersion (SD) systems have been extensively used to increase the dissolution and bioavailability of poorly water-soluble drugs. To circumvent the limitations of polyvinylpyrrolidone (PVP) dispersions, HPMC E5 was applied in the formulation process and scaling-up techniques, simultaneously. In this study, SD of nimodipine (NMP) and corresponding tablets were prepared through solvent method and fluid bed granulating one step technique, respectively. Discriminatory dissolution media were used to obtain reliable dissolution results. Meanwhile, the stability study of SDs was investigated with storage under high temperature and humidity conditions. Moreover, the solubility of SDs was measured to explore the effect of carriers. The preparations were characterized by DSC, PXRD, and FTIR. Dramatical improvements in the dissolution rate of NMP were achieved by the ingenious combination of the two polymers. Binary NMP/PVP/HPMC-SDs released steadily, while the dissolution of single NMP/PVP-SDs decreased rapidly in water. The fluid-bed tablets (FB-T) possessed a similar dissolution behavior to the commercial Nimotop? tablets. The characterization patterns implied that NMP existed in an amorphous state in our SDs. Furthermore, the results of stability tests suggested a better stability of the binary SDs. A special cooperative effect of PVP and HPMC was discovered on dissolution characteristics of NMP SDs and tablets, which could be extended to other drugs henceforth. Finally, the bioavailability of FB-T was evaluated in beagle dogs with Nimotop? as the reference, and the results showed a higher AUC sub0–12h/subvalue for FB-T.
机译：固体分散（SD）系统已被广泛用于增加水溶性差的药物的溶解度和生物利用度。为了避免聚乙烯吡咯烷酮（PVP）分散液的局限性，HPMC E5同时应用于配制工艺和放大技术中。本研究通过溶剂法和流化床造粒一步法分别制备了尼莫地平（NMP）和相应片剂的SD。区别溶出介质用于获得可靠的溶出结果。同时，研究了在高温高湿条件下SDs的稳定性研究。此外，测量SD的溶解度以探索载体的作用。通过DSC，PXRD和FTIR对制剂进行表征。两种聚合物的巧妙组合实现了NMP溶解速率的显着改善。二进制NMP / PVP / HPMC-SDs稳定释放，而单个NMP / PVP-SDs在水中的溶解迅速降低。流化床片剂（FB-T）具有与商业Nimotop®类似的溶解行为。平板电脑。表征模式暗示NMP在我们的SD中以非晶态存在。此外，稳定性测试的结果表明二进制SD具有更好的稳定性。发现PVP和HPMC对NMP SD和片剂的溶出特性具有特殊的协同作用，此后可扩展到其他药物。最后，用Nimotop？评估了比格犬的FB-T的生物利用度。作为参考，结果表明FB-T的AUC 0-12h 值较高。

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